Discovery of a Novel Class of Acylthiourea-Containing Isoxazoline Insecticides against Plutella xylostella

Autor: Fangyi Li, Biaobiao Jiang, Yuqin Luo, Siqi He, Di Feng, Deyu Hu, Runjiang Song
Jazyk: angličtina
Rok vydání: 2023
Předmět:
Zdroj: Molecules, Vol 28, Iss 8, p 3300 (2023)
Druh dokumentu: article
ISSN: 1420-3049
45395756
DOI: 10.3390/molecules28083300
Popis: Isoxazoline structures are widely found in natural products and are rich in biological activities. This study discloses the development of a series of novel isoxazoline derivatives by introducing acylthiourea fragments to access insecticidal activity. All synthetic compounds were examined for their insecticidal activity against Plutella xylostella, with results showing moderate to strong activity. Based on this, the structure–activity relationship analysis was carried out via the constructed three-dimensional quantitative structure–activity relationship model to further guide the structure optimization, resulting in the optimal compound 32. The LC50 of compound 32 against Plutella xylostella was 0.26 mg/L, demonstrating better activity than the positive control, ethiprole (LC50 = 3.81 mg/L), avermectin (LC50 = 12.32 mg/L), and compounds 1–31. The insect GABA enzyme-linked immunosorbent assay demonstrated that compound 32 might act on the insect GABA receptor, and the molecular docking assay further illustrated the mode of action of compound 32 with the GABA receptor. In addition, the proteomics analysis indicated that the action of compound 32 on Plutella xylostella was multi-pathway.
Databáze: Directory of Open Access Journals
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